



| 货号 | 包装规格 | 操作 |
|---|---|---|
| JN0006-5MG | 5 mg | |
| JN0006-25MG | 25 mg |
≥98%(HPLC)
Draflazine (R88021; (-)-R75231), is a potent nucleoside transporter ENT1 (SLC29A1) inhibitor with 370-fold selectivity over ENT2 (SLC29A2). R88021 exhibits 30- and 40-times higher affinity as (+)-R75231 (R88016) using calf lung membrane preparation (by [3H]R75231 & [3H]NBI displacement) and intact human erythrocytes (by [3H]NBMPR displacement), respectively. Draflazine is 20-times more potent as R88016 in enhancing adenosine potency against ADP-induced aggregation in human whole blood (IC50 = 0.5 μM vs 10 μM with 1 μM respective inhibitor), Draflazine and R75231, but not R88016, show cardioprotective efficacy against catecholamines infusion in rabbits in vivo.
强效核苷转运蛋白ENT 1(SLC 29 A1)抑制剂,选择性是ENT 2(SLC 29 A2)的370倍,在体内具有心脏保护功效。
| 英文名称 | Draflazine |
| CAS 号 | 138681-29-5 |
| 经验分子式 | C30H33Cl2F2N5O2 |
| 分子量 | 604.52 |
| UNSPSC | 12352200 |
| NACRES | NA.77 |
| SMILES字符串 | Fc1ccc(cc1)C(CCCCN3CC(N(CC3)CC(=O)Nc4c(cc(cc4Cl)N)Cl)C(=O)N)c2ccc(cc2)F |
| InChI | 1S/C30H33Cl2F2N5O2/c31-25-15-23(35)16-26(32)29(25)37-28(40)18-39-14-13-38(17-27(39)30(36)41)12-2-1-3-24(19-4-8-21(33)9-5-19)20-6-10-22(34)11-7-20/h4-11,15-16,24,27H,1-3,12-14,17-18,35H2,(H2,36,41)(H,37,40) |
| InChI key | IWMYIWLIESDFRZ-UHFFFAOYSA-N |
| 含量测定 | ≥98%(HPLC) |
| 形态 | 粉末 |
| 光学活性 | [α]/D -23 to -29°, c = 0.5 in ethanol |
| 颜色 | 白色至米色 |
| 溶解性 | DMSO: 2 mg/mL,清澈 |
| 储存温度 | 室温 |
| 包装规格(货号 JN0006-5MG) | 5 mg |
| 包装规格(货号 JN0006-25MG) | 25 mg |